MEK-IN-5

MEK-IN-5 is a potent MEK inhibitor and NO donor. MEK-IN-5 significantly reduces the levels of pMEK and pERK in a dose-dependent and time-dependent manner. MEK-IN-5 induces apoptosis in MDA-MB-231 cells[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> MAPK/ERK Pathway >> MEK

MEK-IN-5 (compound 18h) shows anti-proliferation activities for different tumor cells and low toxicity for normal cells[1]. MEK-IN-5 (0.1, 1, 10 µM; 1, 2, 4, 6 h) decreases the expression level of pMEK and pERK in a dose-dependent and time-dependent manner[1]. MEK-IN-5 (1, 10 µM; 24 h) induces apoptosis in MDA-MB-231 cells[1]. MEK-IN-5 (100 µM; 2h) significantly induce NO release in HCT116 cells[1]. Cell Proliferation Assay[1] Cell Line: MDA-MB-231, HCT116, A549, Vero, HL7702 cells Concentration: Incubation Time: Result: Showed anti-proliferation activities in MDA-MB-231, HCT116, A549, Vero, HL7702 cells with IC50s of 0.034, 0.64, 1.35, 21.07, 5.62 µM, respectively. Western Blot Analysis[1] Cell Line: MDA-MB-231 cells Concentration: 0.1, 1, 10 µM Incubation Time: 1, 2, 4, 6 h Result: Decreased the expression level of pMEK and pERK in a dose-dependent and time-dependent manner. Apoptosis Analysis[1] Cell Line: MDA-MB-231 cells Concentration: 1, 10 µM Incubation Time: 24 h Result: Induced apoptosis in MDA-MB-231 cells.

[1]. Wang C, et al. Hybrids of MEK inhibitor and NO donor as multitarget antitumor drugs. Eur J Med Chem. 2020; 196:112271.